Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

A kind of compound and its preparation and use

A compound, phenyl technology, applied in the field of medicine, can solve problems such as toxic side effects and drug resistance

Inactive Publication Date: 2016-03-02
SUZHOU UNIV
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the toxic side effects of traditional drugs and the emergence of drug resistance, it is urgent to develop new anti-myeloma drugs

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A kind of compound and its preparation and use
  • A kind of compound and its preparation and use
  • A kind of compound and its preparation and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0125] The preparation of embodiment 1 compound C98

[0126] 1. Dissolve the compound of structure shown in formula VII (2g, 8.3mmol / L, 1.0eq), malonic acid (1.3g, 12.4mmol / L, 1.5eq) in 20ml of anhydrous pyridine, and drop into morpholine under stirring (72.28mg, 0.8mmol / L, 0.1eq), reflux and stir at 80°C for 24h, add 2mol HCl to the reaction system after the reaction is completed, a large amount of solid precipitates, filter, wash the filter cake with water and a small amount of EA, and dry the filter cake with an infrared lamp , the obtained product 2 is a mixture, and the pale yellow solid is 2.4 g of the structure compound shown in formula VIII, which can be directly used in subsequent reactions.

[0127] Characterization of the structural compound shown in formula VIII: MS: [M-H]-: Foundm / z280.8Calcdm / z281.0

[0128] 2. Suspend the compound of formula VIII (2.4g, 8.48mmol / L, 1.0eq) in the mixed solution of MeOH and DMSO, slowly add SOCl 2 And add DMSO to make the system...

Embodiment 2

[0139] Example 2 Compound C98 inhibits the growth of multiple myeloma cells and leukemia cells

[0140] Culture a variety of multiple myeloma cells: H929, JJN3, KMS11, KMS18, LP1, MM.1S, OCI-MY5, OPM2, RPMI-8226, U266; leukemia cells: K562, Jurkat, AML-2, NB-4, THP-1.

[0141] Treated with different concentrations of C98, the concentrations of C98 were 0.39μmol / L, 0.78μmol / L, 1.56μmol / L, 3.125μmol / L, 6.25μmol / L, 12.5μmol / L, 25μmol / L. After 72 hours of treatment, cell viability was analyzed by MTS / PMS staining.

[0142] figure 2 The effect of different concentrations of C98 compounds on multiple myeloma cells is shown. The results show that C98 has an inhibitory effect on the growth and proliferation of multiple myeloma in a concentration-dependent manner.

[0143] image 3 Effects of different concentrations of C98 compounds on leukemia cells. The results show that C98 has an inhibitory effect on the proliferation and growth of leukemia cells in a concentration-dependent ...

Embodiment 3

[0145] Example 3 Compound C98 induces apoptosis of multiple myeloma cells

[0146] Culture LP1, OPM2, OCI-MY5, JJN3 cells.

[0147] Treat with different concentrations of C98, the concentration of C98 is 0 μmol / L, 2.5 μmol / L, 5 μmol / L in turn, and the cells are collected after 24 hours of treatment, and AnnexinV-FITC (labeled apoptotic cells) and PI (propidium iodide) Double staining, detection of AnnexinV by flow cytometry + percentage of cells. The result is as Figure 4 and as shown in Table 1:

[0148] Table 1 Effects of different concentrations of C98 compounds on apoptosis of myeloma cells

[0149]

[0150] The results showed that: C98 can effectively induce the apoptosis of multiple myeloma cells, and with the increase of C98 drug concentration, the proportion of cells undergoing apoptosis also gradually increased. It shows that the apoptosis rate is concentration-dependent with C98.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to the technical field of medicines, and particularly relates to a compound and a preparation method and application thereof. The compound has a structure shown as a formula I in the specification, is screened out by a computer simulation and molecular docking technology, and has the effects of inhibiting a PI3K (phosphatidyl inositol 3-kinase) path and inhibiting growth and activity of tumors, and the capability of inducing tumor cell apoptosis according to confirmations. Experiments show that the compound can apparently inhibit expression of key enzyme and phosphorylation in the PI3K signal path, the inhibition function has obvious time dependency and concentration dependency, and furthermore, experiments prove that the compound cannot inhibit the key enzyme in other metabolic pathways, but can inhibit the PI3K signal path specifically.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a compound and its preparation and application. Background technique [0002] Multiple myeloma (MM) is a malignant tumor derived from B cells. In recent years, the wide application of new chemotherapy drugs has made great progress in the treatment of multiple myeloma. However, the incidence of this cancer is increasing year by year and showing a trend of younger age. Cancer data report that myeloma is the second most common blood disease and is still considered an incurable disease. Due to the side effects of traditional drugs and the emergence of drug resistance, it is urgent to develop new anti-myeloma drugs. Among them, target-based drug design has become a hot spot for innovative drugs. [0003] The phosphoinositide 3-kinase (PI3K) signaling pathway controls many cell biological processes that are critical in tumorigenesis and development, including apoptosis, transcriptio...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/54C07D207/337C07D333/24A61K31/40A61K31/341A61K31/381A61P35/00
CPCC07D207/337C07D307/54C07D333/24
Inventor 毛新良侯廷军朱景宇乔春华
Owner SUZHOU UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com